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Editorial - ACS Combinatorial Science (ACS Publications)

See also: Strategies for the Use of Mixture-Based Synthetic Combinatorial Libraries: Scaffold Ranking, Direct Testing In Vivo, and Enhanced Deconvolut...
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 Copyright 2008 by the American Chemical Society

Volume 10, Number 1

January/February 2008

Editorial This issue of JCC marks the beginning of our 10th volume. So much change in such a short period of time! Drug discovery programs embraced high-throughput synthesis so quickly that it is now a “given” that library (lead or focused) generation is a regular part of the process (as I presaged back in 1996).1 “The proof of the pudding is in the tasting”. Approximately 235 small molecule pharmaceuticals2 are predicted to sell at least $500 million in 2010. Based on my own survey, at least 60% of them began as hits from a screening library or from a focused library. Those libraries arose primarily as the result of high-throughput synthesis programs conducted by chemists somewhere in the world. As long as high-throughput screening serves as the beginning of a search for drugs, high-throughput synthesis must feed the screens. While there are several ways to conduct highthroughput synthesis, combinatorial chemistry (a “matrix” approach to the preparation of substances) is by far the dominant activity leading to new diversity in compound libraries. As long as humans are unable to predict ligand binding strengths de novo, we will continue to be pleasantly surprised by the results of library screening. The content of JCC increasingly involves combinatorial preparation of both new materials and small molecules with functions other than as pharmaceuticals. I think we did a good job ten years ago setting up the Scope and Editorial Policy. It states The primary objective of the Journal is to publish studies that contribute to a critical understanding of the methods for high-throughput synthesis of substances. The Journal will provide a vehicle for publication in all areas of combinatorial chemistry including synthesis of small organic molecules, macromolecules, and novel materials including polymers, ceramics, metals, etc. In addition, properties such as biological activity as well as interesting materials properties (e.g. superconductivity, optical, electrical) are within the scope of the Journal.

There’s no specific mention of pharmaceuticals here, just molecules with useful functions. I’m proud to see that we are publishing increasing numbers of studies in this Journal

leading to nonpharmaceutical applications, and I have no doubt that this trend will continue. This year will see the re-emergence of an older paper format, the Perspective, and the addition of a paper format new to JCC, the Account. (My thanks to Joan Valentine of Accounts of Chemical Research for graciously consenting to my request.) Our first Account, from Richard Houghten and the team at Torrey Pines Institute for Molecular Studies, premiers in this issue. Manuscripts in these two categories are “by invitation” only. Any ideas for future Perspectives and Accounts should be directed to our office via [email protected]. Anthony W. Czarnik References and Notes (1) Czarnik, A. W. Acc. Chem. Res. 1996, 29, 112–113. (2) Alendronate, alfuzosin, aliskiren, aloglipitin, alvimopan, ambrisentan, amibegron, amlodipine, amoxicillin, anidulafungin, apixaban, aprepitant, arformoterol, aripiprazole, armodafinil, arzoxifene, asenapine, atazanavir, atomoxetine, atorvastatin, atrasentan, axitinib, azithromycin, aztreonam, bazedoxifene, bendamustine, bicalutamide, bifeprunox, bifeprunox, bortezomib, bosentan, bromfenac, budesonide, buprenorphine, bupropion, capecitabine, carvedilol, caspofungin, ceftriaxone, celecoxib, cetirizine, ciclesonide, ciprofloxacin, clarithromycin, clazosentan, clopidogrel, conivaptan, dalbavancin, dapoxetine, darunavir, dasatinib, decitabine, deferasirox, desloratadine, desvenlafaxine, dianicline, diclofenac, disufenton, donepezil, doripenem, doxazosin, dronedarone, dutasteride, efavirenz, eletriptan, eltrombopag, enalapril, entecavir, enzastaurin, eplivanserin, erlotinib, escitalopram, eszopiclone, etodolae, etoricoxib, ezetimibe, famotidine, fenofibrate, fesoterodine, fexofenadine, finasteride, fingolimod, fluconazole, fluticasone, fluvastatin, fondaparinux, fosamprenavir, fosaprepitant, fospropofol, frovatriptan, fulvestrant, gabapentin, gaboxadol, gemcitabine, glimepiride, guanfacine, hydromorphone, ibandronate, iclaprim, imatinib, indiplon, irinotecan, itraconazole, ixabepilone, lamotrigine, lapaquistat, lapatinib, laropiprant, larotaxel, lasofoxifene, latanoprost, lenalidomide, lestaurtinib, letrozole, levalbuterol, levetiracetam, levocetirizine, linezolid, lisdexamfetamine, losartan, lubiprostone, lumiracoxib, lurasidone, maraviroc, memantine, meropenem, methylnaltrexone, methylphenidate, miglustat, milnacipran, modafinil, mometasone, montelukast, moxifloxacin, muraglitazar, mycophenolate mofetil,

10.1021/cc7001759 CCC: $40.75  2008 American Chemical Society Published on Web 01/14/2008

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Journal of Combinatorial Chemistry, 2008 Vol. 10, No. 1 nalmefene, naltrexone, nebivolol, nelarabine, nicaraven, nicorandil, octreotide, odiparcil, olanzapine, olmesartan, olopatadine, ondansetron, oseltamivir, oxaliplatin, oxcarbazepine, oxybutynin, paclitaxel, paclitaxel, paliperidone, palonosetron, pantoprazole, pelitrexol, pemetrexed, pioglitazone, posaconazole, prasugrel, pravastatin, prazosin, pregabalin, quetiapine, radafaxine, raloxifene, ramelteon, ramipril, ranolazine, retapamulin, risedronate, risperidone, rivaroxaban, rivastigmine, ropinirole, rosiglitazone, rosuvastatin, ruboxistaurin, rufinamide, salmeterol xinafoate, saredutant, satavaptan, saxagliptin, senicapoc, sertraline, sildenafil, simvastatin, sitagliptin, sorafenib,

sugammadex, sumatriptan, sunitinib, tacrolimus, tafenoquine, tamsulosin, tapentadol, tazobactam, tegaserod, telaprevir, telavancin, telbivudine, telithromycin, temsirolimus, tenofovir, terbinafine, tesaglitazar, tiagabine, tigecycline, tiotropium, tipranavir, tirapazamine, tolterodine, topiramate, topotecan, trabectedin, tramiprosate, valacyclolvir, valganciclovir, valsartan, varenicline, vernakalant, vildagliptin, vinflunine, viramidine, voriconazole, vorinostat, xaliproden, zanamivir, ziprasidone, zoledronic acid, zolpidem. CC7001759